Journal
ONCOTARGET
Volume 8, Issue 55, Pages 94297-94316Publisher
IMPACT JOURNALS LLC
DOI: 10.18632/oncotarget.21691
Keywords
valsartan; SMEDDS; solid carrier; tablet; optimization
Categories
Funding
- Advanced Technology Center - Ministry of Trade, Industry & Energy (MI, Korea) [10051950]
- Korea Evaluation Institute of Industrial Technology (KEIT) [10051950] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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In order to improve the dissolution and oral bioavailability of valsartan (VST), and reduce the required volume for treatment, we previously formulated a supersaturable self-microemulsifying drug delivery system (SuSMEDDS) composed of VST (80 mg), Capmul (R) MCM (13.2 mg), Tween (R) 80 (59.2 mg), Transcutol (R) P (59.2 mg), and Poloxamer 407 (13.2 mg). In the present study, by using Florite (R) PS-10 (119.1 mg) and Vivapur (R) 105 (105.6 mg) as solid carriers, VST-loaded solidified SuSMEDDS (S-SuSMEDDS) granules were successfully developed, which possessed good flow properties and rapid drug dissolution. By introducing croscarmellose sodium (31 mg) as a superdisintegrant, S-SuSMEDDS tablets were also successfully formulated, which showed fast disintegration and high dissolution efficiency. Preparation of granules and tablets was successfully optimized using D-optimal mixture design and 3-level factorial design, respectively, resulting in percentage prediction errors of < 10%. In pharmacokinetic studies in rats, the relative bioavailability of the optimized granules was 107% and 222% of values obtained for SuSMEDDS and Diovan (R) powder, respectively. Therefore, we conclude that novel S-SuSMEDDS formulations offer great potential for developing solid dosage forms of a liquefied formulation such as SuSMEDDS, while improving oral absorption of drugs with poor water solubility.
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